Icotinib hydrochloride is a National Class 1.1 new drug that is independently developed by Betta Pharmaceuticals Co., Ltd. for nearly a decade. It is also China's first small molecule targeted anti-cancer drug. Icotinib is a potent and highly selective oral epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI), and it is used for the first-line treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) patients carrying EGFR mutations. 

lung cancer

Ensartinib is a novel, potent and highly selective next-generation inhibitor of anaplastic lymphoma kinase (ALK), which has a potency more than ten-times greater than crizotinib in enzymatic assays. Ensartinib targets ALK, inhibiting downstream malignant pathways that contribute to tumorigenesis and disease progression. Ensatinib has shown good efficacy in in vitro and in vivo studies, including those tumors that are already resistant to clozatinib, and has inhibitory effects on c-Met, TRK 1/ 2/ 3, ROS1, etc. A phase III head to head trial is evaluating ensartinib as the first-line treatment in patients with ALK-positive non-small cell lung cancer as compared with crizotinib.

colorectal cance

Bevacizumab (MIL60) is a targeted antibody drug against human vascular endothelial growth factor (VEGF), a biosimilar to Bevacizumab injection, and can be used to treat non-small cell lung cancer, colorectal cancer, and several other solid tumor indications. Bevacizumab inhibits tumor angiogenesis by inhibiting the binding of VEGF to the vascular endothelial cell surface receptor (VEGFR), thereby cutting off tumor feeding to stop tumor growth.Bevacizumab was officially approved for marketing in November 2021 for the indications of metastatic colorectal cancer and advanced, metastatic or recurrent non-small cell lung cancer. In March 2022 Bevacizumab was approved for several New indications (recurrent glioblastoma, epithelial ovarian cancer, fallopian tube cancer or primary peritoneal cancer, etc.) were approved.

lung cancer, colorectal cancer

BPI-D0316 is a 3rd-generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) targeting T790M mutation. Studies have shown that 3rd-gen EGFR-TKI targeting T790M mutation can significantly improve patients' quality of life and prolong overall survival. On May 31st, 2023, Befotertinib Mesylate Capsule was approved by the NMPA.

renal cell carcinoma

Vorolanib (CM082) is a novel next-generation of multi-target kinase inhibitor, which can inhibit tumor angiogenesis and growth, and can be used in the treatment of many kinds of cancer. Vorolanib has a significant anti-angiogenic effect on VEGFR, PDGFR, c-Kit, Flt-3, CSF1R and other multiple targets, and the special PK/PD of vorolanib can preserve activity and reduce toxicity. A phase II/III clinical trial (CONCEPT) is evaluating vorolanib in combination with everolimus in the treatment of patients with advanced renal cell carcinoma.

lung cance

Balstilimab is a human monoclonal antibody targeting programmed cell death protein 1 (PD-1), and is an immune checkpoint inhibitor. Balstilimab potently antagonizes PD-1 binding to PD-L1 and PD-L2, relieves T cell suppression, and enhances T cell effector function, therefore activating the immune system to attack tumor. Balstilimab as a single agent and in combination with Zalifrelimab, an anti-CTLA-4 antibody, is planned for clinical investigation for the treatment of advanced cervical cancer as well as other advanced solid tumors. The IND applications for Balstilimab have been accepted by NMPA CDE and are currently in technical review.

Zalifrelimab is a human monoclonal antibody targeting cytotoxic T-lymphocyte associated protein 4 (CTLA-4), and is an immune checkpoint inhibitor. By blockade of CTLA-4 binding to its ligands, CD80 and CD86, Zalifrelimab antagonizes the negative regulation of T cells by CTLA-4, therefore enhancing tumor immune surveillance and anti-tumor response. Zalifrelimab is planned for clinical investigation in combination with Balstilimab, an anti-PD-1 antibody, for the treatment of advanced cervical cancer as well as other advanced solid tumors. The IND applications for Zalifrelimab have been accepted by NMPA CDE and are currently in technical review.

BPI-16350 is a novel antitumor drug independently developed by Betta. It is a cyclin dependent kinase CDK4 and CDK6 inhibitor with new structure. CDK4/6 are the key factors to regulate cell cycle, which can trigger cell cycle transition from G1 phase to S phase. BPI-16350 can specifically combine with CDK4/6 to inhibit the kinase activity, inhibit the proliferation, metastasis and other related signal transduction of cancer cells, block the cell cycle in G1 phase, thus inhibiting the proliferation of tumor cells. The clinical trial of BPI-16350 in breast cancer has been approved and is now ongoing.

melanoma

MRX2843 is a novel, potent,  and bioavailable small-molecule oral inhibitor, which is a dual inhibitor of MERTK and FLT3. MERTK and FLT3 are overexpressed or mutated in a variety of tumors. MRX2843 can affect tumor growth by inhibiting MERTK and FLT3 in tumor cells and innate immune cells in tumor microenvironment, thereby affecting the key signal transduction pathways or immunomodulation to inhibit tumors. The clinical trial of MRX2843 for advanced solid tumor has been approved, and it is ongoing.

solid tumors, hematological malignancies

BPI-361175 is a novel, oral, highly potent and selective 4th generation EGFR inhibitor developed by Betta Pharmaceutical Co., Ltd. The new chemical entity targets EGFR C797S mutation and other EGFR related mutations that are resistant to 3rd generation EGFR TKI in non-small cell lung cancer (NSCLC) and other solid tumors. It shows excellent inhibitory effect and selectivity in vitro assay and exhibits significant anti-tumor activity in a variety of xenograft models harboring EGFR C797S or other related mutations. The IND application of BPI-361175 has been approved by NMPA, and Phase 1 clinical trial is being initiated.

BPI-21668 is a novel, potent and selective small molecule inhibitor of Phosphatidylinositol 3-kinase α (PI3Kα) developed by Betta Pharma. It is intended to be used for the treatment of advanced solid tumor with PIK3CA mutations. BPI-21668 shows consistent biological activities in vitro and in vivo. It can potently and selectively inhibit proliferation of PIK3CA-mutant cells. Used as a single agent or in combination, BPI-21668 shows good anti-tumor effect in multiple solid tumor models. BPI-21668 also exhibits excellent physicochemical and pharmacokinetic properties. The IND application of BPI-21668 has been approved by NMPA, and Phase 1 clinical trial is starting.

MCLA-129 is a bispecific antibody targeting both EGFR and c-Met. MCLA-129 can simultaneously block the signal transductions of EGFR and c-MET, therefore inhibiting tumor growth and survival. Through enhanced ADCC and ADCP activities, MCLA-129’s tumor cell killing potential is further increased. MCLA-129 is planned for clinical investigation for the treatment of advanced solid tumors with EGFR or MET abnormalities. The clinical trial for MCLA-129 has been approved and is currently under development.

BPI-371153 is a new molecular entity compound developed by Beda Pharmaceuticals, which is a novel potent and highly selective oral small molecule PD-L1 inhibitor, intended for the treatment of patients with locally advanced or metastatic solid tumors or relapsed/refractory lymphoma. Preclinical data show that BPI-371153 can effectively induce and stabilize PD-L1 dimer formation and endocytosis, thereby potently blocking PD-L1/PD-1 interactions. Currently, the BPI-371153 drug clinical trial application has been approved and is well underway.

BPI-442096 is a new molecular entity with full intellectual property rights developed by Beda Pharmaceutical Co., Ltd. and is a novel potent and highly selective oral small molecule inhibitor of Src homology region 2 domain-containing phosphatase-2 (SHP2). BPI-442096 inhibits the activation of SHP2 by specifically targeting the SHP2 protein variable configuration site, thereby inhibiting the signaling pathways including RAS-MAPK and PD-L1/PD-1, thereby inhibiting the proliferation, growth, survival, motility and metabolism of tumor cells, and ultimately achieving the goal of tumor growth inhibition. Currently, BPI-442096 was approved for clinical trials in China on January 24, 2022 and in the U.S. on May 20, 2022, and the clinical trials in China and the U.S. are progressing smoothly.

BPI-452080 is a new molecular entity compound with fully independent intellectual property rights developed by Betta Pharmaceuticals. It is a highly efficient and specific small molecule HIF-2α (Hypoxia inducible factor-2α) inhibitor, intended for the treatment of patients with advanced solid tumors. Preclinical studies have shown that BPI-452080 can specifically block the heterodimerization of HIF-2α and HIF-1β, thereby inhibiting the transcriptional expression of downstream genes, and exhibits excellent in vitro activity and in vivo efficacy with good pharmacokinetic properties and safety in a variety of tumor cells and animal models with abnormal hypoxia or oxygen-sensing pathways. Currently, the clinical trial of BPI-452080 has been approved in January 2023 and is now well underway.

BPB-101 Dual Antibody Injection is the first new First-in-class (FIC) macromolecule drug developed by Betta Pharmaceuticals. It is a bispecific IgG1 subtype humanized antibody with triple function, intended for the treatment of patients with a variety of advanced solid tumors, including but not limited to non-small cell lung cancer, ovarian cancer, breast cancer, esophageal cancer, melanoma, endometrial cancer, bladder cancer, bile duct cancer, colorectal cancer, liver cancer and other cancers. Preclinical studies have shown that BPB-101 can specifically target the GARP-TGF-β complex, mature TGF-β, and PD-L1, thereby relieving the dual immunosuppression of the TGF-β signaling axis and PD-1/PD-L1 signaling axis of the tumor microenvironment, restoring and enhancing the efficacy of immune cells in killing tumor cells, and thus inhibiting the growth and survival of tumor. Currently, BPB-101 is approved for clinical trials in March 2023 and is well underway.

BPI-460372 is a new molecular entity compound targeting the Hippo signaling pathway, which is a novel potent transcriptional enhanced associate domain (TEAD) small molecule inhibitor, developed by Betta Pharmaceutical Co. Preclinical studies have demonstrated the excellent in vitro and in vivo activity, excellent pharmacokinetic properties and good safety profile of BPI-460372. The clinical trials of BPI-460372 in China and America have been approved in January 2023 and are now well underway.

BPI-472372 is a new molecular entity compound with fully independent intellectual property rights developed by Betta Pharmaceuticals. It is a highly efficient and specific small molecule CD73 inhibitor, intended for the treatment of patients with advanced solid tumors. Preclinical studies have shown that BPI-472372 can specifically inhibit CD73 nuclease activity, downregulate adenosine levels in the tumor microenvironment, and exert anti-tumor effects by relieving tumor immunosuppression. It has demonstrated excellent in vitro and in vivo activity, pharmacokinetic properties and good safety profile in preclinical studies. BPI-472372 is currently approved for clinical trials in March 2023 and is well underway.

EYP-1901 is an investigational long-acting treatment for wet AMD, non proliferative diabetic retinopathy (NPDR), diabetic macular edema (DME) and pmCNV that combines the active drug vorolanib with Durasert™, an approved intravitreal drug delivery system from EyePoint Pharmaceuticals. Durasert is delivered via a single injection in the physician’s office, and it has been safely administered to thousands of patients' eyes across four U.S. FDA approved products. EYP-1901 uses an erodible formulation of EyePoint's proprietary Durasert delivery technology (Durasert E™) and can achieve sustained release for approximately 9 months .

CFT8919 is an orally bioavailable allosteric BiDAC™ degrader. CFT8919 is active in in vitro and in vivo models of EGFR L858R-driven NSCLC. It can target EGFR drug-resistance secondary mutations and exhibits intracranial activity, which has the potential to prevent or treat brain metastasis. CFT8919 tablet has been approved for clinical trials, and its development is ongoing.

BPI-221351 is a new chemical entity developed by Betta, with full intellectual property rights. It is a novel, brain-penetrant, highly potent, highly selective IDH1 and IDH2 mutant selective small molecule dual inhibitor, intended for solid tumor patients carrying IDH1 and IDH2 mutations including but not limited to glioblastoma and biliary tract cancers and etc..

BPI-520105 is a new chemical entity developed by Betta, with full intellectual property rights. It is a novel, highly potent pan-EGFR inhibitor, with high selectivity towards multiple EGFR mutations, targeting EGFR mutations in solid tumor patients.